Issue 5, 2013
From the journal:

MedChemComm

Development of a diketopiperazine-forming dipeptidyl Gly-Pro spacer for preparation of an antibody–drug conjugate†

Shino Manabe,*a   Hikaru Machida,b   Yoshiyuki Aihara,a   Masahiro Yasunaga,b   Yukishige Itoa  and  Yasuhiro Matsumura*b  

* Corresponding authors

a RIKEN, Advanced Science Institute, Synthetic Cellular Chemistry Laboratory, Hirosawa, Wako, Saitama 351-0198, Japan
E-mail: smanabe@riken.jp
Fax: +81 48 462 4680
Tel: +81 48 467 9432

b Investigative Treatment Division, Research Center for Innovative Oncology, National Cancer Center Hospital East, Kashiwa, Chiba 277-0882, Japan
E-mail: yhmatsum@east.ncc.go.jp
Fax: +81 4713 6857
Tel: +81 4713 6857

Abstract

We developed a novel diketopiperazine-forming dipeptidyl spacer aimed at application in antibody–drug conjugates. Enzymatic cleavage of a peptide linked to the Gly-Pro spacer resulted in formation of diketopiperazine, which was stable and non-toxic, and release of the parent drug.

Graphical abstract: Development of a diketopiperazine-forming dipeptidyl Gly-Pro spacer for preparation of an antibody–drug conjugate

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Article information

DOI
https://doi.org/10.1039/C3MD00075C
Article type
Concise Article
Submitted
05 Mar 2013
Accepted
05 Mar 2013
First published
06 Mar 2013

Med. Chem. Commun., 2013,4, 792-796

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Development of a diketopiperazine-forming dipeptidyl Gly-Pro spacer for preparation of an antibody–drug conjugate

S. Manabe, H. Machida, Y. Aihara, M. Yasunaga, Y. Ito and Y. Matsumura, Med. Chem. Commun., 2013, 4, 792 DOI: 10.1039/C3MD00075C

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